Verhoef J C, Boddé H E, de Boer A G, Bouwstra J A, Junginger H E, Merkus F W, Breimer D D
Center for Bio-Pharmaceutical Sciences, Leiden University, The Netherlands.
Eur J Drug Metab Pharmacokinet. 1990 Apr-Jun;15(2):83-93. doi: 10.1007/BF03190191.
The transport characteristics of peptide and proteins drugs across various epithelial membrane barriers are outlines. These include transport through the intestinal, buccal, nasal and pulmonary absorptive mucosae, as well as transdermal penetration. Because peptides and proteins are hydrophilic and high molecular weight compounds, they commonly show minor permeability across the mentioned biological membranes. In order to improve their transport properties and thereby their systemic bioavailability, several strategies can be undertaken, such as the synthesis of stabilized and lipophilic analogues, the application of absorption enhancers and protease inhibitors, and the design of suitable dosage forms (e.g., liposomes, biodegradable nanocapsules, bioadhesive microspheres).
概述了肽类和蛋白质类药物跨各种上皮膜屏障的转运特性。这些包括通过肠道、口腔、鼻腔和肺部吸收性黏膜的转运,以及透皮渗透。由于肽类和蛋白质类是亲水性高分子量化合物,它们通常在上述生物膜上表现出较小的渗透性。为了改善它们的转运特性从而提高其全身生物利用度,可以采取几种策略,例如合成稳定的亲脂性类似物、应用吸收促进剂和蛋白酶抑制剂,以及设计合适的剂型(如脂质体、可生物降解纳米胶囊、生物黏附微球)。